| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| AdipoRon | Axon 2275
CAS [924416-43-3]
MF C27H28N2O3MW 428.52
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Orally active small-molecule AdipoR agonist (Kd values 1.8 and 3.1 μM for AdipoR1 and AdipoR2 respectively) that exerts antidiabetic effects via activation of AMPK and PPAR-α pathways.AdipoRon ameliorated insulin resistance, glucose intolerance, and diabetes of genetically obese rodent model db/db mice, thereby prolonging the shortened lifespan of db/db mice on a high-fat diet.
References
Certificates
Categories
Extra info
M. Okada-Iwabu et al. A small-molecule AdipoR agonist for type 2 diabetes and short life in obesity. Nature. 2013, 503, 493-499.
Y.T. Ang et al. PAQR proteins: a novel membrane receptor family defined by an ancient 7-transmembrane pass motif. J. Mol. Evol. 2005, 61, 372-380.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Diabetes & Metabolism
PI3K-Akt-mTOR
AdipoR1
AdipoR2
PAQR1
Orally active small-molecule AdipoR agonist
Chemical name
2-(4-benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide
Parent CAS No.
[924416-43-3]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| INT 131 - AMG 131 | Axon 2019
CAS [315224-26-1]
MF C21H12Cl4N2O3SMW 514.21
Purity:
99%
Soluble in DMSO
Description
Highly potent, non-TZD, selective peroxisome proliferator-activated receptor gamma (“PPAR-γ“) modulator (SPPARM); INT131 is a PPAR-γ partial agonist and potential therapeutic agent for the treatment of type 2 diabetes
References
Certificates
Categories
Extra info
A Motani et al. INT131: a selective modulator of PPAR gamma. J. Mol. Biol. 2009, 386(5), 1301-1311.
JP Taygerly et al. Discovery of INT131: A selective PPARγ modulator that enhances insulin sensitivity. Bioorg. Med. Chem. 2013, 21(4), 979–992.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
PPAR
NR1C
Selective PPARγ modulator (partial agonist)
Chemical name
2,4-dichloro-N-(3,5-dichloro-4-(quinolin-3-yloxy)phenyl)benzenesulfonamide
Parent CAS No.
[315224-26-1]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| GSK 3787 | Axon 1628
CAS [188591-46-0]
MF C15H12ClF3N2O3SMW 392.78
Purity:
99%
Soluble in DMSO
Description
Selective and irreversible peroxisome proliferator-activated receptor (PPARδ) antagonist
References
Certificates
Categories
Extra info
PS Palkar et al. Cellular and Pharmacological Selectivity of the PPARβ/δ Antagonist GSK3787. Mol. Pharmacol. Fast Forward. 2010.06.01.
BG Shearer et al. Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible PPARdelta antagonist. J. Med. Chem. 2010, 53(4), 1857-61.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
PPAR
NR1C
PPARδ antagonist
Chemical name
4-chloro-N-(2-(5-(trifluoromethyl)pyridin-2-ylsulfonyl)ethyl)benzamide
Parent CAS No.
[188591-46-0]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| GW 7647 | Axon 1237
CAS [265129-71-3]
MF C29H46N2O3SMW 502.75
Purity:
99%
Soluble in DMSO and Ethanol
Description
Potent and selective Peroxisome proliferator-activated receptor-α (PPARα) agonist
KEYWORDS: GW 7647 | supplier | PPARα agonist | GW7647 | CAS [265129-71-3] | Metabolism | PPAR | Agonist | Peroxisome | proliferator-activated | PPARα | lipids | fatty acid | | axonmedchem |
| WY 14643 | Axon 1227
CAS [50892-23-4]
MF C14H14ClN3O2SMW 323.80
Purity:
98%
Soluble in DMSO
Description
Selective PPARα agonist
References
Certificates
Categories
Extra info
Forman et al. Hypolipidemic drugs, polyunsaturated fatty acids, and eicosanoids are ligands for peroxisome proliferator-activated receptors α and d. Proc. Natl. Acad. Sci. USA 1997, 94, 4312.
Bishop-Bailey. Peroxisome proliferator-activated receptors in the cardiovascular system. Br. J. Pharmacol. 2000, 129, 823.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
PPAR
NR1C
PPARα agonist
Chemical name
[4-Chloro-6-(2,3-dimethyl-phenylamino)-pyrimidin-2-ylsulfanyl]-acetic acid
Parent CAS No.
[50892-23-4]
Order
Size
Unit Price
Stock
10 mg
€45.00
In Stock | | axonmedchem |
| KRP 297 - MK 767 | Axon 1567
CAS [213252-19-8]
MF C20H17F3N2O4SMW 438.42
Purity:
98%
Soluble in DMSO
Description
Peroxisome proliferator-activated receptor (PPAR) alpha and gamma (PPARα and PPARγ) agonist
References
Certificates
Categories
Extra info
AC Calkin et al. MK-767. Kyorin/Banyu/Merck. Curr Opin Investig Drugs. 2003, 4(4), 444-8.
M Nomura et al. (3-Substituted benzyl)thiazolidine-2,4-diones as structurally new antihyperglycemic agents. Bioorg. Med. Chem. Lett. 1999, 9(4), 533.
K Murakami et al. A novel insulin sensitizer acts as a coligand for PPAR-alpha and PPAR-gamma: effect of PPAR-alpha activation on abnormal lipid metabolism in liver of Zucker fatty rats. Diabetes 1998, 47(12), 1841-1847.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
PPAR
NR1C
PPARα agonist; PPARγ agonist
Chemical name
5-(2,4-Dioxo-thiazolidin-5-ylmethyl)-2-methoxy-N-(4-trifluoromethyl-benzyl)-benzamide
Parent CAS No.
[213252-19-8]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| CHIR 99021 dihydrochloride - CT 99021 dihydrochloride | Axon 2435
CAS [N.A.]
MF C22H18Cl2N8.2HClMW 538.26
Purity:
99%
Soluble in water and DMSO
Description
Very potent and specific glycogen synthase kinase GSK-3 inhibitor; highly recommended tool. Water soluble hydrochloride salt of CHIR 99021 (Axon 1386, parent molecule)
* CHIR99021 and PD0325901 (Axon 1408) are often used together as 2i in stem cell research (Axon 2128).
*Promotion | | axonmedchem |
| WAY 262611 dihydrochloride | Axon 2188
CAS [N.A.]
MF C20H22N4.2HClMW 391.34
Purity:
99%
Soluble in water and DMSO
Description
Inhibitor of Dickkopf-1 (DKK1); WAY 262611 is a wingless Wnt/β-Catenin signaling agonist with an inhibitory effect on DKK1, displaying an EC50 value of 0.63 μM for DKK1-mediated TCF-Luciferase, no affinity for GSK-3β (IC50 value >100 μM) and enhancing the bone formation rate in ovariectomized (OVX) rats following oral adminstration. Dickkopf-1 (DKK1) is a soluble inhibitor of Wnt-3a mediated Wnt/β-catenin signaling required for embryonic head development. It regulates Wnt signaling by binding to the Wnt coreceptor lipoprotein-related protein-5 (LRP5)/Arrow, and Kremen2 (Kr2) simultaneously.
References
Certificates
Categories
Extra info
J.C. Pelletier et al. (1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate. J. Med. Chem. 2009, 52, 6962-6965.
J.J. Pinzone et al. The role of Dickkopf-1 in bone development, homeostasis, and disease. Blood 2009, 113, 517-525.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
Wnt-β-Catenin
Wnt
Inhibitor of Dickkopf-1 (DKK1); Wnt/β-Catenin signaling agonist
Chemical name
(1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine dihydrochloride
Parent CAS No.
[1123231-07-1]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| Wnt agonist 1 | Axon 2120
CAS [853220-52-7]
MF C19H18N4O3MW 350.37
Purity:
99%
Soluble in DMSO and Ethanol
Description
A cell permeable and selective Wnt signaling pathway agonist or activator. It mimics the effects of a Wnt ligand in a Xenopus model and may be a useful tool in the study of physiol. processes that involve the Wnt pathway; it induces in vitro β-catenin and transcription factor (TCF) dependent transcriptional activity in 293T cells in a dose dependent manner with an EC50 of 0.7 mM
References
Certificates
Categories
Extra info
J Liu et al. A small-molecule agonist of the Wnt signaling pathway. Angew. Chem. Int. Ed. Engl. 2005, 44(13), 1987-1990.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Stem Cell
β-Catenin
Wnt-β-Catenin
Cell-Cell Adhesion Protein
Wnt
Wnt/β-catenin signaling pathway agonist or activator
Chemical name
N4-(benzo[d][1,3]dioxol-5-ylmethyl)-6-(3-methoxyphenyl)pyrimidine-2,4-diamine
Parent CAS No.
[853220-52-7]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| iCRT5 - CRT Inhibitor iCRT5 | Axon 2133
CAS [18623-44-4]
MF C16H17NO5S2MW 367.44
Purity:
99%
Soluble in DMSO
Description
Potent and cell-permeable β-catenin-responsive transcription (CRT) inhibitor, with IC50 value of 18 nM for Wnt responsive STF16 luciferase (STF16-Luc). iCRT5 acts by disrupting the interaction between β-catenin and TCF4, possibly by direct binding to β-catenin, while displaying minimal or less prominent effect on non-canonical Wnt signaling and other pathways such as Hh, JAK/STAT, and Notch signaling
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
β-Catenin
Wnt-β-Catenin
Cell-Cell Adhesion Protein
Wnt
β-Catenin-responsive transcription (CRT) inhibitor
Chemical name
4-(5-(3,4-dimethoxybenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)butanoic acid
Parent CAS No.
[18623-44-4]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| KY 05009 | Axon 2395
CAS [1228280-29-2]
MF C18H16N4O2SMW 352.41
Purity:
99%
Soluble in DMSO
Description
Inhibitor of Traf2- and Nck-Interacting Kinase (TNIK; Ki value 100 nM in ATP-competitive assay) that attenuates TGF-β1-mediated Wnt and Smad signaling and epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma A549 cells. Additionally, KY05009 inhibits TGF-β1-induced phosphorylation of JNK1/2, FAK, Src, and paxillin.
References
Certificates
Categories
Extra info
J. Kim et al. A novel aminothiazole KY-05009 with potential to inhibit Traf2- and Nck-interacting kinase (TNIK) attenuates TGF-β1-mediated epithelial-to-mesenchymal transition in human lung adenocarcinoma A549 cells. PLoS One. 2014 Oct 22;9(10):e110180.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Wnt-β-Catenin
NF-κB
TGF-β
MAPK
EC 2.7.11.1
TNIK
Inhibitor of TNIK that attenuates TGF-β1-mediated Wnt and Smad signaling
Chemical name
5-(4-methylbenzamido)-2-(phenylamino)thiazole-4-carboxamide
Parent CAS No.
[1228280-29-2]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| JW 55 | Axon 1922
CAS [664993-53-7]
MF C25H26N2O5MW 434.48
Purity:
99%
Soluble in DMSO
Description
A tankyrase (TNKS) inhibitor, inhibiting PARP domain of TNKS1 and TNKS2; JW55 inhibits canonical Wnt signaling in colon carcinoma cells and reduces tumor growth in conditional APC mutant mice
References
Certificates
Categories
Extra info
J Waaler et al. A novel tankyrase inhibitor decreases canonical Wnt signaling in colon carcinoma cells and reduces tumor growth in conditional APC mutant mice. Cancer Res. 2012, 72(11), 2822-32.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Stem Cell
Wnt-β-Catenin
DNA-damage Response
EC 2.4.2.30
TNKS
Inhibitor of tankyrase (TNKS 1 and 2)
Chemical name
N-(4-((4-(4-methoxyphenyl)tetrahydro-2H-pyran-4-yl)methylcarbamoyl)phenyl)furan-2-carboxamide
Parent CAS No.
[664993-53-7]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| ICG 001 | Axon 1766
CAS [847591-62-2]
MF C33H32N4O4MW 548.63
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Specific inhibitor of Wnt/β-catenin signaling pathway; inhibiting β-catenin/cyclic AMP response element-binding (CREB) protein transcription. ICG-001 selectively induces apoptosis in transformed cells but not in normal colon cells, reduces in vitro growth of colon carcinoma cells, and is efficacious in the Min mouse and nude mouse xenograft models of colon cancer
References
Certificates
Categories
Extra info
KH Emami et al. A small molecule inhibitor of β-catenin/cyclic AMP response element-binding protein transcription. PNAS 2004, 101(34), 12682-12687.
M Eguchi et al. ICG-001, a novel small molecule regulator of TCF/beta-catenin transcription. Med. Chem. 2005, 1(5), 467-472.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Stem Cell
β-Catenin
Wnt-β-Catenin
Cell-Cell Adhesion Protein
Wnt
Specific inhibitor of Wnt/β-catenin signaling pathway
Chemical name
(6S,9aS)-N-benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxooctahydro-1H-pyrimido[1,2-a]pyrazine-1-carboxamide
Parent CAS No.
[780757-88-2 (relative stereochemistry; Scifinder names incorrectly)
847591-62-2 (absolute stereochemistry)]
Order
Size
Unit Price
Stock
5 mg
€115.00
In Stock | | axonmedchem |
| BIO - GSK-3 inhibitor IX | 6-Bromoindirubin-3'-oxime | Axon 1693
CAS [667463-62-9]
MF C16H10BrN3O2MW 356.17
Purity:
98%
Soluble in DMSO
Description
Potent, reversible, ATP-competitive and selective inhibitor of glycogen synthase kinase GSK-3 (IC50: 5 nM); Inhibition of GSK by BIO results in the activation of the Wnt signaling pathway and sustained pluripotency in human and murine embryonic stem cells (ESCs). BIO is shown to maintain self-renewal in human and murine ESCs
References
Certificates
Categories
Extra info
N Sato et al. Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor. Nature Med. 2004, 10(1), 55-63.
L Meijer et al. GSK-3-selective inhibitors derived from tyrian purple indirubins. Chem. Biol. 2003, 10, 1255-1266.
AS Tseng et al. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes. Chem. Biol. 2006, 13, 957.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
GSK-3
Wnt-β-Catenin
PI3K-Akt-mTOR
EC 2.7.11.26
GSK-3 inhibitor
Chemical name
(Z)-6'-Bromo-1H,1'H-[2,3']biindolylidene-3,2'-dione 3-oxime
Parent CAS No.
[667463-62-9]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| REP 3123 dihydrochloride - CRS3123 dihydrochloride | Axon 1705
CAS [1013915-99-5]
MF C19H19Br2N3O2S.2HClMW 586.17
Purity:
99%
Optical purity:
>98% ee
Soluble in DMSO
Description
Selective inhibitor of methionyl-tRNA synthetase (MetRS); agent to treat Clostridium difficile infection (CDI); Antibiotic.
KEYWORDS: REP 3123 dihydrochloride | supplier | MetRS inhibitor | CRS3123 dihydrochloride | REP3123 dihydrochloride | REP-3123 dihydrochloride | CRS 3123 dihydrochloride | CRS-3123 dihydrochloride | CAS [1013915-99-5 ] | [1013915-71-3 (absolute | (+)-rotamer)] | DNA-RNA | MetRS | Inhibitor | Enzymes | | axonmedchem |
| GANT61 - NSC 136476 | Axon 2642
CAS [500579-04-4]
MF C27H35N5MW 429.60
Purity:
99%
Soluble in DMSO and Ethanol
Description
Small molecule capable of reducing GLI-mediated transcription and endogenous Hedgehog (Hh) signaling (IC50 value ca 5 µM). In vivo, GANT61 suppressed human tumor cell growth until no tumor was palpable.
KEYWORDS: GANT61 | supplier | GLI inhibitor | NSC 136476 | GANT-61 | NSC136476 | CAS [500579-04-4] | Hedgehog | GLI1 | GLI2 | Transcription Factor | Hh | Hedgehog signaling | cancer | cytotoxic | AML | tumor | apoptosis | leukemia | | axonmedchem |
| REP 8839 | Axon 1704
CAS [757942-43-1]
MF C20H21BrFN3OSMW 450.37
Purity:
99%
Soluble in DMSO
Description
Selective inhibitor of methionyl-tRNA synthetase (MetRS) with antibacterial activity against a variety of gram-positive organisms; Antibiotic
References
Certificates
Categories
Extra info
LS Green et al. Inhibition of Methionyl-tRNA Synthetase by REP8839 and Effects of Resistance Mutations on Enzyme Activity. Antimicrob. Agents Chemother. 2009, 86–94.
IA Critchley et al. Antibacterial Activity of REP8839, a New Antibiotic for Topical Use. Antimicrob. Agents Chemother. 2005, 49(10), 4247–4252.
UA Ochsner et al. Mode of Action and Biochemical Characterization of REP8839, a Novel Inhibitor of Methionyl-tRNA Synthetase. Antimicrob Agents Chemother. 2005, 49(10), 4253–4262.
IA Critchley and UA Ochsner. Recent advances in the preclinical evaluation of the topical antibacterial agent REP8839. Curr. Opin. Chem. Biol. 2008, 12(4), 409-417.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
MetRS
EC 6.1.1.10
Antibiotics
MetRS inhibitor
Chemical name
2-(3-((4-bromo-5-(1-fluorovinyl)-3-methylthiophen-2-yl)methylamino)propylamino)quinolin-4(1H)-one
Parent CAS No.
[757942-43-1]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| Azithromycin - CP 62993 | Zithromax | Axon 2042
CAS [117772-70-0]
MF C38H72N2O12MW 748.98
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Macrolide antibiotic; inhibits bacterial protein synthesis through binding to the 50S ribosomal subunit; one of the world's best-selling antibiotics
References
Certificates
Categories
Extra info
R.M. Gilhotra et al. Azithromycin novel drug delivery system for ocular application. Int. J. Pharm. Investig. 2011, 1, 22-28.
Certificate of Analysis
Material Safety Data Sheet
Immunology
EC 2.3.2.12
Peptidyl Transferase
Pfizer Licensed Products
Antibiotics
Macrolide antibiotic; Binds the 50S ribosomal subunit
Chemical name
(2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-11-((2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yloxy)-2-ethyl-3,4,10-trihydroxy-13-((2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yloxy)-3,5,6,8,10,12,14-heptamethyl-1
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[83905-01-5]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| KU 0060648 | Axon 2604
CAS [881375-00-4]
MF C33H34N4O4SMW 582.71
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases.
* The 3HCl salt of KU 0060648 (Axon 1584) used to be available as well, but is discontinued (Autumn 2016)
KEYWORDS: KU 0060648 | Supplier | DNA-PK inhibitor | KU0060648 | CAS [881375-00-4] | DNA-RNA | DNA-PK | Inhibitor | PIKK | PI3K | cancer | DNA repair | DSB | double-strand breaks | | axonmedchem |
| PNU 100480 - PF 02341272 | U 100480 | Sutezolid | Axon 1762
CAS [168828-58-8]
MF C16H20FN3O3SMW 353.41
Purity:
99%
Soluble in DMSO
Description
Antituberculosis (anti-TB) agent under clinical development; potent inhibitor of bacterial protein biosynthesis by interfering with the binding of initiator fMet-tRNA(i)(Met) to the ribosomal peptidyltransferase P-site
References
Certificates
Categories
Extra info
KN Williams et al. Promising Antituberculosis Activity of the Oxazolidinone PNU-100480 Relative to That of Linezolid in a Murine Model. Antimicrob Agents Chemother. 2009, 53(4), 1314–1319.
KN Williams et al. Addition of PNU-100480 to first-line drugs shortens the time needed to cure murine tuberculosis. Am. J. Respir. Crit. Care Med. 2009, 180(4), 371-6.
U Patel et al. Oxazolidinones mechanism of action: inhibition of the first peptide bond formation. J. Biol. Chem. 2001, 276(40), 37199-205.
CE Barry and JS Blanchard. The Chemical Biology of New Drugs in Development for Tuberculosis. Curr. Opin. Chem. Biol. 2010, 14(4), 456–466.
Certificate of Analysis
Material Safety Data Sheet
Immunology
EC 2.3.2.12
Peptidyl Transferase
Pfizer Licensed Products
Ribosomal peptidyl transferase center (PTC) inhibitor
Chemical name
(S)-N-((3-(3-fluoro-4-thiomorpholinophenyl)-2-oxooxazolidin-5-yl)methyl)acetamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[168828-58-8]
Order
Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| VE 822 | Axon 2452
CAS [1232416-25-9]
MF C24H25N5O3SMW 463.55
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Selective ATR inhibitor (IC50 values 0.019 µM, 2.6 µM, and 18.1 µM for ATR, ATM, and DNA-PK, respectively) with in vitro and in vivo activity that decreases maintenance of cell-cycle checkpoints and homologous recombination in irradiated cancer cells, and increases persistent DNA damage. VE822 decreased survival of pancreatic cancer cells but not normal cells in response to XRT or gemcitabine.
References
Certificates
Categories
Extra info
E. Fokas et al. Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation. Cell Death Dis. 2012 Dec 6;3:e441.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
ATR
p53-Tumor Suppression
PI3K-Akt-mTOR
DNA-damage Response
EC 2.7.11.1
Selective ATR inhibitor that decreases survival of pancreatic cancer cells
Chemical name
5-(4-(isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine
Parent CAS No.
[1232416-25-9]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| AS 252424 bispotassium salt - AS 252424K | Axon 1436
CAS [N.A.]
MF C14H6FNO4S.K2MW 381.46
Purity:
99%
Soluble in water and DMSO
Description
Potent and selective PI3K p110γ inhibitor; IC50 values for inhibition of human recombinant PI3Kγ, α, β, and δ to be 30, 940, 20,000, and 20,000 nM respectively; water-soluble bispotassium salt form of AS 252424 (Axon 1424).
References
Certificates
Categories
Extra info
V. Pomel et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. J. Med. Chem. 2006, 49, 3857-3871.
T. Rückle et al. PI3Kgamma inhibition: towards an 'aspirin of the 21st century'? Nat. Rev. Drug Discov. 2006, 5, 903-918.
B.T. Hennessy et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nat. Rev. Drug Discov. 2005, 4, 988-1004.
A.M. Condliffe et al. Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils. Blood. 2005, 106, 1432-1440.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
PI3K inhibitor (p110-γ specific)
Chemical name
Bispotassium 5-[1-[5-(4-Fluoro-2-hydroxy-phenyl)-furan-2-yl]-meth-(Z)-ylidene]-thiazolidine-2,4-dione
Parent CAS No.
[900515-16-4]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| CZC 24832 | Axon 2039
CAS [1159824-67-5]
MF C15H17FN6O2SMW 364.40
Purity:
99%
Soluble in DMSO
Description
Potent and selective PI3K p110γ inhibitor, with efficacy in in vitro and in vivo models of inflammation
References
Certificates
Categories
Extra info
G Bergamini et al. A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation. Nat. Chem. Biol. 2012, 8(6), 576-582.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Pain & Inflammation
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
PI3K inhibitor (p110-γ specific)
Chemical name
5-(2-amino-8-fluoro-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-tert-butylpyridine-3-sulfonamide
Parent CAS No.
[1159824-67-5]
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Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| CAL 101 - Idelalisib | Axon 2170
CAS [870281-82-6]
MF C22H18FN7OMW 415.42
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Orally active and selective inhibitor of PI3K δ-isoform (IC50 p110δ: 2.5nM), displaying clinical activity in chronic lymphocytic leukemia (CLL). Cal 101 is 40- to 300-fold more selective for PI3K-δ (δ) isoform relative vs other PI3K class I enzymes (p110α, p110β, and p110γ IC50 were 820, 565, and 89nM, respectively). It does not promote apoptosis in normal T cells or natural killer cells, nor does it diminish antibody-dependent cellular cytotoxicity.
References
Certificates
Categories
Extra info
S.E.M. Herman et al. Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood 2010, 116, 2078-2088.
J. Hoellenriegel et al. The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood 2011, 118, 3603-3612.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Pain & Inflammation
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
PI3K inhibitor (p110 δ specific)
Chemical name
(S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one
Parent CAS No.
[870281-82-6]
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Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| GSK 2636771 dihydrochloride | Axon 1912
CAS [1372540-25-4]
MF C22H22F3N3O3.2HClMW 506.35
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Potent, orally available and specific PI3K p110β (PI3K beta, PI3Kβ) inhibitor
References
Certificates
Categories
Extra info
RA Rivero, MA Hardwick. Identification of GSK2636771, a potent and selective, orally bioavailable inhibitor of phosphatidylinositol 3-kinase-beta (PI3Kβ) for the treatment of PTEN deficient tumors. Cancer Res. 2012, 72(8 Supplement), 2913.
RM Sanchez et al. Synthesis and structure–activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent β isoform selective phosphatidylinositol 3-kinase inhibitors. Bioorg. Med. Chem. Lett. 2012, 22(9), 3198-3202.
H Lin. Isoform Selective PI3K-beta Inhibitors. Chin. J. Chem. 2013, 31(3), 299-303.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
PI3K inhibitor (p110 β specific)
Chemical name
2-methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acid dihydrochloride
Parent CAS No.
[1372540-25-4]
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Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| IC 87114 | Axon 2168
CAS [371242-69-2]
MF C22H19N7OMW 397.43
Purity:
98%
Soluble in DMSO
Description
Potent and highly selective small molecule inhibitor of the PI3K p110δ isoform (IC50 values for PI3Kα, β, γ, and δ are >100, 75, 29, and 0.5 μM respectively). IC87114 potently inhibited PIP3 biosynthesis in neutrophils by 60–65% and at 1 μM, it inhibited neutrophil migration by 75% as compared with the control.IC 87114 reduced the infiltration of inflammatory cells into the pancreatic islets and, accordingly, delayed and reduced the loss of glucose homeostasis.
References
Certificates
Categories
Extra info
C. Sadhu et al. Essential role of phosphoinositide 3-kinase delta in neutrophil directional movement. J. Immunol. 2003, 170, 2647-2654.
D.P. Sutherlin et al. Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf. Bioorg. Med. Chem. Lett. 2012, 22, 4296-302.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Pain & Inflammation
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
Potent and highly selective inhibitor of the PI3K p110δ
Chemical name
2-((6-amino-9H-purin-9-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one
Parent CAS No.
[371242-69-2]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| Trovafloxacin mesylate - CP 99219 mesylate | Axon 2100
CAS [147059-75-4]
MF C20H15F3N4O3.CH4O3SMW 512.46
Purity:
100%
Soluble in water and DMSO
Description
Antibiotic. Inhibits bacterial DNA gyrase and topoisomerase IV and DNA gyrase; DNA synthesis inhibitor
References
Certificates
Categories
Extra info
AA Khan et al. Trovafloxacin is active against Toxoplasma gondii. Antimicrob. Agents Chemother. 1996, 40, 1855-1859.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
DNA-damage Response
EC 5.99.1.3
TOPO
Pfizer Licensed Products
Inhibitor of bacterial DNA gyrase and Topo IV
Chemical name
7-((1R,5S,6s)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid compound with methanesulfonic acid (1:1)
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[147059-72-1]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| CHIR 124 | Axon 1636
CAS [405168-58-3]
MF C23H22ClN5OMW 419.91
Purity:
98%
Optical purity:
>98% ee
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, cell permeable and selective Chk1 inhibitor (IC50: 0.32 nM and 697 nM for Chk1 and Chk2 respectively).
KEYWORDS: CHIR 124 | supplier | CHK1 inhibitor | CHIR124 | CHIR-124 | CAS [405168-58-3] | DNA-RNA | CHK | Checkpoint | p53 | cell cycle | DNA damage | arrest | apoptosis | | axonmedchem |
| Genz 644282 | Axon 2198
CAS [529488-28-6]
MF C22H21N3O5MW 407.42
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Topoisomerase I inhibitor (IC50 value 0.4 nM in human bone marrow CFU-GM assay). Cytotoxic agent, with activity toward 8 human tumor cell lines of varied histology and resistance mechanisms by colony formation, with enhanced potency compared to topotecan and SN-38. Contrary to the camptothecins, Genz-644282 is not a substrate for the multidrug resistance gene 1 (MDR1) and breast cancer resistance protein (BCRP) efflux pumps.
References
Certificates
Categories
Extra info
L.S. Kurtzberg et al. Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment. Clin. Cancer Res. 2011, 17, 2777-2787.
P.J. Houghton et al. Testing of the topoisomerase 1 inhibitor Genz-644282 by the pediatric preclinical testing program. Pediatr. Blood Cancer. 2012, 58, 200-209.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
DNA-damage Response
EC 5.99.1.2
TOPO
Topo I inhibitor lacking MDR1 and BCRP affinity
Chemical name
2,3-Dimethoxy-12-(2-(methylamino)ethyl)-[1,3]dioxolo[4',5':4,5]benzo[1,2-h]benzo[c][1,6]naphthyridin-13(12H)-one
Parent CAS No.
[529488-28-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Homocamptothecin, (±)-E- - hCPT, dl- | BN 80245 | Axon 1687
CAS [186668-40-6]
MF C21H18N2O4MW 362.38
Purity:
99%
Optical purity:
racemate
Moderately soluble in DMSO
Description
A potent topoisomerase I (Topo 1) inhibitor; Homocamptothecin (hCPT) is an E-ring modified analogue of camptothecin (CPT), with enhanced stability and potent Topo-1 mediated activity; apoptosis agent
References
Certificates
Categories
Extra info
L Lesueur-Ginot et al. Homocamptothecin, an E-ring modified camptothecin with enhanced lactone stability, retains topoisomerase I-targeted activity and antitumor properties. Cancer Res. 1999, 59(12), 2939-2943.
O Lavergne et al. Homocamptothecins: Synthesis and Antitumor Activity of Novel E-Ring-Modified Camptothecin Analogues. J. Med. Chem. 1998, 41(27), 5410–5419.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
DNA-damage Response
EC 5.99.1.2
TOPO
Potent topoisomerase I (Topo 1) inhibitor
Chemical name
3H,15H-Oxepino[3',4':6,7]indolizino[1,2-b]quinoline-3,15-dione, 5-ethyl-1,4,5,13-tetrahydro-5-hydroxy-
Parent CAS No.
[186668-40-6]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| PF 477736 - PF 00477736 | Axon 1379
CAS [952021-60-2]
MF C22H25N7O2MW 419.48
Purity:
98%
Optical purity:
99% ee
Soluble in DMSO
Description
Chk1 inhibitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity
References
Certificates
Categories
Extra info
JW Janetka et al, Inhibitors of Checkpoint Kinases: From discovery to the clinic. Curr. Opin. Drug Discov. & Devel. 2007, 10(4), 473-486.
S. Ashwell and S Zabludoff. DNA Damage Detection and Repair Pathways Recent Advances with Inhibitors of Checkpoint Kinases in Cancer Therapy. Clin. Cancer Res. 2008, 14(13), 4033-4037.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Stem Cell
p53-Tumor Suppression
DNA-damage Response
EC 2.7.11.1
CHK
Pfizer Licensed Products
CHK1 inhibitor
Chemical name
(R)-2-Amino-2-cyclohexyl-N-[2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-5,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl]-acetamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[952021-60-2]
Order
Size
Unit Price
Stock
2 mg
€70.00
In Stock | | axonmedchem |
| Bizine | Axon 2306
CAS [N.A.]
MF C18H23N3O.HClMW 333.86
Purity:
98%
Soluble in water and DMSO
Description
Potent LSD1 inhibitor in vitro and selective versus monoamine oxidases A/B and the LSD1 homologue, LSD2 with Ki(inact) values 0.059 μM, 2.6 μM, 6.5 μM, and ca 11 μM for LSD1, MAO-A, MAO-B, and LSD2 respectively. Bizine was found to be effective at modulating bulk histone methylation in cancer cells. Moreover, neurons exposed to oxidative stress were protected by the presence of bizine, suggesting potential applications in neurodegenerative disease.
References
Certificates
Categories
Extra info
P. Prusevich et al. A selective phenelzine analogue inhibitor of histone demethylase LSD1. ACS Chem. Biol. 2014, 9, 1284-1293.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Epigenetics
Immunology
EC 1.14.11
Histone demethylase
Potent LSD1 inhibitor with selectivity over MAO-A/B, and LSD2
Chemical name
N-(4-(2-hydrazinylethyl)phenyl)-4-phenylbutanamide hydrochloride
Parent CAS No.
[1591932-50-1]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| YUKA1 | Axon 2674
CAS [708991-09-7]
MF C13H16N4O2SMW 292.36
Purity:
99%
Soluble in DMSO
Description
YUKA1 is a cell-permeable selective inhibitor of lysine demethylase 5A (KDM5A/RBP2/JARID1A) (IC50 value 2.66 μM). YUKA1 blocks drug resistance and cancer cell growth in HeLa cervical cancer cells and ZR-75-1 breast cancer cells. YUKA1 was able to increase H3K4me3 levels in human cells and selectively inhibited the proliferation of cancer cells whose growth depends on KDM5A.
KEYWORDS: YUKA1 | supplier | KDM5A inhibitor | YUKA-1 | YUKA 1 | CAS [708991-09-7] | Histone | Histone demethylase | Inhibitor | Enzymes | KDM5A | RBP2 | JARID1A | | axonmedchem |
| JIB 04 - NSC 693627 | Axon 2160
CAS [199596-05-9]
MF C17H13ClN4MW 308.76
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, cell permeable and selective Jumonji histone demethylase inhibitor in vitro and in vivo; JIB-04 is not a competitive inhibitor of α-ketoglutarate and it modulates transcription in cancer-selective manner
References
Certificates
Categories
Extra info
L Wang et al. A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth. Nat. Commun. 2013, 4, 2035.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
EC 1.14.11
Histone demethylase
Antibiotics
Jumonji histone demethylase inhibitor
Chemical name
(E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine
Parent CAS No.
[199596-05-9]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| MK 1775 - AZD 1775 | Adavosertib | Axon 1494
CAS [955365-80-7]
MF C27H32N8O2MW 500.60
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
A potent and selective Wee1 kinase inhibitor in vitro and in vivo. MK 1775 abolishes cyclin-dependent kinase 1 (CDC2) activity by phosphorylation of the Tyr15 residue. It abrogates a DNA damage checkpoint (G2-phase), leading to apoptosis in combination with several DNA-damaging agents selectively in p53-deficient tumor cell lines. It is under clinical trial for advanced solid tumors.
KEYWORDS: MK 1775 | supplier | Wee1 inhibitor | AZD 1775 | Adavosertib | supplier | MK1775 | AZD1775 | CAS [955365-80-7] | CDK1 | Wee1 | Inhibitor | cyclin-dependent kinase 1 | CDC2 | DNA damage | checkpoint | G2-phase | apoptosis | p53-deficient | solid tumor | | axonmedchem |
| ML 324 dihydrochloride | Axon 2081
CAS [N.A.]
MF C21H23N3O2.2HClMW 422.35
Purity:
100%
Soluble in water and DMSO
Description
Inhibitor of Jumonji domain-containing protein 2 (JMJD2, an "eraser") histone demethylase; effectively blocked herpes simplex virus (HSV) IE gene expression and prevented viral reactivation from latency; >75 fold more efficient than DMOG
References
Certificates
Categories
Extra info
Y Liang et al. Targeting the JMJD2 histone demethylases to epigenetically control herpesvirus infection and reactivation from latency. Sci Transl Med. 2013, 5(167), 167ra5.
C Harrison. Comment in Epigenetic drugs: new modulators of readers and erasers. Nat. Rev. Drug Discov. 2013, 12(3), 188.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
EC 1.14.11
Histone demethylase
Inhibitor of JMJD2 histone demethylase
Chemical name
N-(3-(dimethylamino)propyl)-4-(8-hydroxyquinolin-6-yl)benzamide dihydrochloride
Parent CAS No.
[1222800-79-4]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| GSK J1 | Axon 1934
CAS [1373422-53-7]
MF C22H23N5O2MW 389.45
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
The first selective and potent histone demethylase JMJD3/UTX inhibitor; blocks demethylation of histone H3K27; showed no activity against a panel of JMJ family demethylases and 100 protein kinases.Available also a cell permeable ethyl ester derivative GSK J4 (Axon 1933), which is a prodrug suitable for cell-based studies and will be hydrolyzed to GSK-J1 in cells rapidly
References
Certificates
Categories
Extra info
L Kruidenier et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 2012, 488(7411), 404-408.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
EC 1.14.11
Histone demethylase
Histone demethylase JMJD3/UTX inhibitor
Chemical name
3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoic acid
Parent CAS No.
[1373422-53-7]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| GSK J4 | Axon 1933
CAS [1373423-53-0]
MF C24H27N5O2MW 417.50
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Histone demethylase JMJD3/UTX inhibitor; blocks demethylation of histone H3K27; As a cell permeable ethyl ester derivative of GSK J1 (Axon 1934), it is a suitable prodrug form for cell-based studies. It is rapidly hydrolyzed in cells, generateing pharmacologically relevant intracellular concentrations of GSK-J1
References
Certificates
Categories
Extra info
L Kruidenier et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 2012, 488(7411), 404-408.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
EC 1.14.11
Histone demethylase
Histone demethylase JMJD3/UTX inhibitor
Chemical name
ethyl 3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate
Parent CAS No.
[1373423-53-0]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| LEE 011 - Ribociclib | Axon 2273
CAS [1211441-98-3]
MF C23H30N8OMW 434.54
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Orally bioavailable and highly selective small-molecule inhibitor of CDK4/6 (mean IC50 value 307 nM in sensitive neuroblastoma-derived cell lines). LEE011 caused cell-cycle arrest and cellular senescence that was attributed to dose-dependent decreases in phosphorylated RB and FOXM1, respectively. LEE 011 treatment of BE2C and IMR5 neuroblastoma cell lines with demonstrated sensitivity to CDK4/6 inhibition resulted in a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle.
KEYWORDS: LEE 011 | supplier | CDK4/6 inhibitor | Ribociclib | LEE011 | LEE-011 | CAS [1211441-98-3] | Cyclin Dependent | CDK4 | CDK6 | orally bioavailable | cell-cycle arrest | senescence | FOXM1 | | axonmedchem |
| Palbociclib isethionate - PD 0332991 isethionate | Axon 2052
CAS [827022-33-3]
MF C24H29N7O2.C2H6O4SMW 573.66
Purity:
99%
Soluble in water and DMSO
Description
An orally active cyclin-dependent kinase (CDK) inhibitor, specifically targeting on CDK4 and CDK6; a potential agent for the treatment of breast cancer.
Another salt form, PD 0332991 hydrochloride (Axon 1505) is also available.
References
Certificates
Categories
Extra info
Malini Guha. Blockbuster dreams for Pfizer's CDK inhibitor. Nature Biotech. 2013, 31, 187.
RL Sutherland and EA Musgrove. CDK inhibitors as potential breast cancer therapeutics: new evidence for enhanced efficacy in ER+ disease. Breast Cancer Res. 2009, 11(6), 112-113.
RS Finn et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009, 11(5), R77.
DW Fry et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol. Cancer Ther. 2004, 3, 1427-1438.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
p53-Tumor Suppression
EC 2.7.11.22
CDK
Pfizer Licensed Products
Orally active cyclin-dependent kinase (CDK4/6) inhibitor
Chemical name
6-acetyl-8-cyclopentyl-5-methyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one 2-hydroxyethanesulfonate
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[571190-30-2]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| PTC 209 | Axon 2420
CAS [315704-66-6]
MF C17H13Br2N5OSMW 495.19
Purity:
99%
Soluble in DMSO
Description
Inhibitor of the canonical self-renewal regulator BMI-1, a vital part of the polycomb repressive complex 1 (PRC1; IC50 value 0.5 µM for inhibition of UTR-mediated luciferase BMI-1 reporter expression). Treatment of primary colorectal cancer xenografts with PTC209 resulted in colorectal CIC loss with long-term and irreversible impairment of tumor growth. PTC-209 preferentially inhibits the proliferation of human lymphoma U937 and HT1080 tumor cells, and is less effective in primary human peripheral blood mononuclear cells and human hematopoietic stem cells.
References
Certificates
Categories
Extra info
A. Kreso et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Stem Cell
Hedgehog
Wnt-β-Catenin
PI3K-Akt-mTOR
DNA-damage Response
Ubiquitin
BMI-1
Inhibitor of the canonical self-renewal regulator BMI-1
Chemical name
N-(2,6-dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)thiazol-2-amine
Parent CAS No.
[315704-66-6]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| XL 413 hydrochloride - BMS 863233 hydrochloride | Axon 2268
CAS [1169562-71-3]
MF C14H12ClN3O2.HClMW 326.18
Purity:
99%
Soluble in water and DMSO
Description
Potent, selective and orally bioavailable CDC7 inhibitor (IC50 value of 3.4 nM) that shows >60-fold selectivity against CK2, >10-fold selectivity against PIM1, and >300-fold selectivity against a panel of over 100 protein kinases. XL 413 induces tumor cell apoptosis and inhibition of tumor cell proliferation in CDC7-overexpressing tumor cells.Further development of XL 413 was terminated due to an unfavorable pharmacological profile observed in phase 1 clinical evaluation.
References
Certificates
Categories
Extra info
R. Swords et al. Cdc7 kinase - a new target for drug development. Eur. J. Cancer. 2010, 46, 33-40.
E.S. Koltun et al. Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg. Med. Chem. Lett. 2012, 22, 3727-3371.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
DNA-damage Response
EC 2.7.11.1
CDC7
Potent, selective and orally bioavailable CDC7 inhibitor
Chemical name
(S)-8-Chloro-2-(pyrrolidin-2-yl)benzofuro[3,2-d]pyrimidin-4(3H)-one hydrochloride
Parent CAS No.
[1169558-38-6]
Order
Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| R 547 | Axon 1983
CAS [741713-40-6]
MF C18H21F2N5O4SMW 441.45
Purity:
99%
Soluble in DMSO
Description
Potent and selective CDK inhibitor with Ki values to be 1, 3, 1 nM for CDK1, CDK2, and CDK4 respectively; inactive (Ki >5000 nM) against a panel of >120 unrelated kinases. R547 effectively inhibits proliferation of tumor cell lines independent of multidrug resistant status, histologic type, retinoblastoma protein, or p53 status, with IC50 values smaller or equal to 0.60 µM in vitro.
References
Certificates
Categories
Extra info
XJ Chu et al. Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with (...). J. Med. Chem. 2006, 49(22), 6549-6560.
W DePinto et al. In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials. Mol. Cancer Ther. 2006, 5(11), 2644-2658.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
p53-Tumor Suppression
EC 2.7.11.22
CDK
CDK inhibitor (1, 2, and 4 specific)
Chemical name
(4-amino-2-(1-(methylsulfonyl)piperidin-4-ylamino)pyrimidin-5-yl)(2,3-difluoro-6-methoxyphenyl)methanone
Parent CAS No.
[741713-40-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| EED226 | Axon 2701
CAS [2083627-02-3]
MF C17H15N5O3SMW 369.40
Purity:
99%
Soluble in DMSO
Description
EED226 is a first-in-class, potent, selective and orally bioavailable PRC2 inhibitor (IC50 values of 23.4 nM and 53.5 nM with H3K27me0 peptide and the mononucleosome as the substrates, respectively) that directly binds to the H3K27me3 binding pocket of EED. EED226 effectively induced tumor regression in a mouse xenograft model.
KEYWORDS: EED226 | supplier | PRC2 inhibitor | EED-226 | EED 226 | CAS [2083627-02-3] | PRC | Inhibitor | Proteins | EED | PRC | EZH1 | EZH2 | | axonmedchem |
| AZD 5438 | Axon 1966
CAS [602306-29-6]
MF C18H21N5O2SMW 371.46
Purity:
99%
Soluble in DMSO
Description
Potent and orally bioavailable inhibitor of cyclin-dependent kinase (cdk) 1, 2, and 9 (IC50: 16, 6, and 20 nM, respectively); AZD5438 showed significant antiproliferative activity in human tumor cell lines (IC50: 0.2-1.7 mM)
References
Certificates
Categories
Extra info
KF Byth et al. AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. Mol. Cancer Ther. 2009, 8(7), 1856-1866.
DS Boss et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of the oral cyclin-dependent kinase inhibitor AZD5438 when administered at intermittent and continuous dosing schedules in patients (...). Ann. Oncol. 2010, 21(4), 884-894.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
p53-Tumor Suppression
EC 2.7.11.22
CDK
CDK inhibitor (1, 2, and 9 specific)
Chemical name
4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)-N-(4-(methylsulfonyl)phenyl)pyrimidin-2-amine
Parent CAS No.
[602306-29-6]
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Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| SCH 727965 - Dinaciclib | Axon 1776
CAS [779353-01-4]
MF C21H28N6O2MW 396.49
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective cyclin-dependent kinase (CDK) inhibitor, selectively inhibiting CDK1, CDK2, CDK5 and CDK9 with IC50 values of 3, 1, 1 and 4 nM respectively; a potential antineoplastic agent
References
Certificates
Categories
Extra info
LS Chen et al. Pim kinase inhibitor, SGI-1776, induces apoptosis in CLL lymphocytes. Blood, 2009, 114 (19), 4150-4157.
SM Mumenthaler et al. Pharmacologic inhibition of Pim kinases alters prostate cancer cell growth and resensitizes chemoresistant cells to taxanes. Mol. Cancer Ther. 2009, 8(10), 2882-2893.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
p53-Tumor Suppression
EC 2.7.11.22
CDK
CDK inhibitor (1, 2, 5, and 9 specific)
Chemical name
(S)-3-((3-ethyl-5-(2-(2-hydroxyethyl)piperidin-1-yl)pyrazolo[1,5-a]pyrimidin-7-ylamino)methyl)pyridine 1-oxide
Parent CAS No.
[779353-01-4]
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Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| AT 7519 mesylate | Axon 1539
CAS [902135-89-1]
MF C16H17Cl2N5O2.CH4O3SMW 478.35
Purity:
99%
Soluble in water
Description
A small molecule inhibitor of multi-CDK, which inhibits CDK 1, 2 , 4, 5, 6, and 9 in vitro and induces apoptosis in multiple myeloma via GSK-3β activation and RNA polymerase II inhibition
References
Certificates
Categories
Extra info
L Sato et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3β activation and RNA polymerase II inhibition. Oncogene 2010, 29, 2325-2336.
MS Squires et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol. Cancer Ther. 2010, 9(4), 920-928.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
p53-Tumor Suppression
EC 2.7.11.22
CDK
CDK inhibitor
Chemical name
4-(2,6-Dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide methanesulfonic acid
Parent CAS No.
[844442-38-2]
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Stock
10 mg
€80.00
In Stock | | axonmedchem |
| PHA-767491 | Axon 2690
CAS [845714-00-3]
MF C12H11N3OMW 213.24
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
PHA-767491 is an ATP mimetic dual CDC7/CDK9 kinase inhibitor (IC50 values of 10 nM and 34 nM for CDC7 and CDK9, respectively). Treatment with PHA-767491 results in apoptotic cell death in multiple cancer cell types and tumor growth inhibition in preclinical cancer models. PHA-767491 is also a potent kinase inhibitor of MAPKAP-K2 (or MK-2) (IC50 value of 171 nM).
KEYWORDS: PHA-767491 | supplier | CDC7/CDK9 inhibitor | PHA767491 | PHA 767491 | CAS [845714-00-3] | DNA-RNA | CDC7 | CDK9 | Inhibitor | Enzymes | [942425-68-5] | MK-2 | MAPKAPK2 | | axonmedchem |
| SNS 032 - BMS 387032 | Axon 1614
CAS [345627-80-7]
MF C17H24N4O2S2MW 380.53
Purity:
99%
Soluble in DMSO
Description
Specific and potent inhibitor of cyclin-dependent kinases (CDK) 2, 7 and 9 (IC50 values to be 38, 4 and 62 nM for cdk2, cdk7 and cdk9 respectively and no activity against 190 additional kinases); SNS 032 induces cell cycle arrest and apoptosis in tumor cell lines
References
Certificates
Categories
Extra info
DS Williamson et al. Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2. Bioorg. Med. Chem. Lett. 2005, 15(4), 863-867.
R Chen et al. Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood, 2009, 113(19), 4637-4645.
WG Tong et al. Phase I and Pharmacologic Study of SNS-032, a Potent and Selective Cdk2, 7, and 9 Inhibitor, in Patients With Advanced Chronic Lymphocytic Leukemia and Multiple Myeloma. J. Clin. Oncol. 2010, 28(18), 3015-3022.
MA Dickson and GK Schwartz. Development of cell-cycle inhibitors for cancer therapy. Curr. Oncol. 2009, 16(2), 36-43.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
p53-Tumor Suppression
EC 2.7.11.22
CDK
CDK inhibitor (2, 7 and 9 specific)
Chemical name
N-(5-((5-tert-butyloxazol-2-yl)methylthio)thiazol-2-yl)piperidine-4-carboxamide
Parent CAS No.
[345627-80-7]
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Size
Unit Price
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5 mg
€85.00
In Stock | | axonmedchem |
| NSC 625987 | Axon 1243
CAS [141992-47-4]
MF C15H13NO2SMW 271.33
Purity:
98%
Soluble in DMSO
Description
Selective and potent cyclin-dependent kinase (CDK) 4 inhibitor
References
Certificates
Categories
Extra info
A Kubo et al. The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4. Clin. Cancer Res. 1999, 5, 4279-4286.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
p53-Tumor Suppression
EC 2.7.11.22
CDK
CDK4 inhibitor
Chemical name
1,4-Dimethoxy-10H-acridine-9-thione
Parent CAS No.
[141992-47-4]
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Size
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Stock
10 mg
€95.00
In Stock | | axonmedchem |